Investigational New Drugs

, Volume 31, Issue 1, pp 230–246 | Cite as

Development of artemisinin compounds for cancer treatment

  • Henry C. Lai
  • Narendra P. Singh
  • Tomikazu Sasaki


Artemisinin contains an endoperoxide moiety that can react with iron to form cytotoxic free radicals. Cancer cells contain significantly more intracellular free iron than normal cells and it has been shown that artemisinin and its analogs selectively cause apoptosis in many cancer cell lines. In addition, artemisinin compounds have been shown to have anti-angiogenic, anti-inflammatory, anti-metastasis, and growth inhibition effects. These properties make artemisinin compounds attractive cancer chemotherapeutic drug candidates. However, simple artemisinin analogs are less potent than traditional cancer chemotherapeutic agents and have short plasma half-lives, and would require high dosage and frequent administration to be effective for cancer treatment. More potent and target-selective artemisinin-compounds are being developed. These include artemisinin dimers and trimers, artemisinin hybrid compounds, and tagging of artemisinin compounds to molecules that are involved in the intracellular iron-delivery mechanism. These compounds are promising potent anticancer compounds that produce significantly less side effect than traditional chemotherapeutic agents.


Artemisinins Anticancer properties Drug development 



The authors’ research on artemisinin was supported by the Breast Cancer Funding of California, the Akibene Foundation, Holley Holdings, Susan Komen for the Cure, the Meryl and Charles Witmer Foundation, the Washington Technology Center, and the Life Sciences Discovery Fund of the State of Washington.

Conflict of interest statement

The authors are co-inventors of technologies, of which the patents are owned by the University of Washington, related to artemisinin-tagged transferrin, artemisinin-tagged transferrin receptor binding peptides, and artemisinin-dimer hydrazone. These technologies are licensed to Holley Pharmaceuticals (China) and Artemisia Biomedical (USA) for commercial development.


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Copyright information

© Springer Science+Business Media, LLC 2012

Authors and Affiliations

  • Henry C. Lai
    • 1
  • Narendra P. Singh
    • 1
  • Tomikazu Sasaki
    • 2
  1. 1.Departments of BioengineeringUniversity of WashingtonSeattleUSA
  2. 2.Departments of ChemistryUniversity of WashingtonSeattleUSA

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